title: Inhibitors of an essential mycobacterial cell wall lipase (Rv3802c) as tuberculosis drug leads.
abstract: The first targeted inhibitors of an essential M. tuberculosis cell wall lipase, Rv3802c, are described. Lead compounds exhibited nanomolar inhibition of the enzyme, and encouraging antibacterial activity against M. tuberculosis in vitro, supporting Rv3802c as a novel TB drug target.
authors.affiliation: Centenary Institute of Cancer Medicine and Cell Biology, Newtown, NSW 2042, Australia.
authors.forename: Nicholas P
authors.initials: NP
authors.lastname: West
authors.forename: Katie M
authors.initials: KM
authors.lastname: Cergol
authors.forename: Millie
authors.initials: M
authors.lastname: Xue
authors.forename: Elizabeth J
authors.initials: EJ
authors.lastname: Randall
authors.forename: Warwick J
authors.initials: WJ
authors.lastname: Britton
authors.forename: Richard J
authors.initials: RJ
authors.lastname: Payne
mesh_terms: D000900:Anti-Bacterial Agents / Q000037:antagonists & inhibitors* / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000037:antagonists & inhibitors* / Q000494:pharmacology*; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors*; D002473:Cell Wall / Q000187:drug effects*; D015195:Drug Design; D006801:Humans; D008049:Lipase / Q000037:antagonists & inhibitors*; D009161:Mycobacterium / Q000187:drug effects*; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000201:enzymology; D014376:Tuberculosis / Q000382:microbiology*
chemical_list: D000900:Anti-Bacterial Agents; D000995:Antitubercular Agents; D001426:Bacterial Proteins; D008049:Lipase